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Antitumor activity of Z-ajoene, a natural compound purified from garlic: antimitotic and microtubule-interaction properties

Title: Antitumor activity of Z-ajoene, a natural compound purified from garlic: antimitotic and microtubule-interaction properties
Authors: Li, Min; Ciu, Jing-Rong; Ye, Ying; Min, Ji-Mei; Zhang, Li-He; Wang, Kui; Gares, Michèle; Cros, Jean; Wright, Michel; Leung-Tack, Jeanne
Publisher Information: Oxford University Press
Publication Year: 2002
Collection: HighWire Press (Stanford University)
Subject Terms: MOLECULAR EPIDEMIOLOGY
Description: Ajoene, a garlic stable oil-soluble sulfur rich compound was generally isolated as a mixture of two isomers [( E, Z )-4,5,9-trithiadodeca-1,6,11-triene-9-oxide]. It has been described essentially as a potent inhibitor of platelet aggregation in vitro and in vivo . The antiproliferative effects of ajoene and experiments using a single isomer had received little attention. The present study aims at defining the antitumor activities of cis - Z -ajoene in vitro and in vivo. Antiproliferative activity of Z -ajoene was demonstrated against a panel of human tumor cell lines with IC 50 values varying from 5.2 mM to 26.1 mM and at a lower extent in normal marsupial kidney cells (PtK2). Meanwhile, Z -ajoene arrested HL60 cells in G 2 /M phase of cell cycle in a dose and time-dependent way. In PtK2 cells, exposure to 20 μM Z -ajoene for 6 h induced a complete disassembly of the microtubule network, that was associated with an increased number of cells blocked in early mitotic stages. An IC 50 for microtubule disassembly of 1 μM was determined by a fully automated microplate-based multi-detection reader. In vitro , a reversible inhibition of the microtubule protein assembly was observed with an IC 50 of 25 μM Z -ajoene. In vivo, Z -ajoene inhibited tumor growth by 38% and 42% in mice grafted with sarcoma 180 and hepatocarcinoma 22, respectively. For the first time, Z -ajoene was shown to be a potent inhibitor of tumor cell growth both in vitro and in vivo . The microtubule cytoskeleton appeared to be one of the Z -ajoene targets, but the mechanisms by which Z -ajoene interacted with microtubule appeared different from those of other microtubule poisons such as those of the Vinca alkaloids family. The ability of Z -ajoene to preferentially suppress the growth of neoplastic cells could provide a new approach in tumor therapy.
Document Type: text
File Description: text/html
Language: English
Relation: http://carcin.oxfordjournals.org/cgi/content/short/23/4/573; http://dx.doi.org/10.1093/carcin/23.4.573
DOI: 10.1093/carcin/23.4.573
Availability: http://carcin.oxfordjournals.org/cgi/content/short/23/4/573; https://doi.org/10.1093/carcin/23.4.573
Rights: Copyright (C) 2002, Oxford University Press
Accession Number: edsbas.82EA5DA1
Database: BASE